Assay Detail
Binding
CHEMBL1953791
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Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.75 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.00 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 6.92 |
| CHEMBL1951070 | — | — | 1 | 6.60 |
| CHEMBL1951069 | — | — | 1 | 6.59 |
| CHEMBL1951067 | — | — | 1 | 6.58 |
| CHEMBL1951066 | — | — | 1 | 6.56 |
| CHEMBL1951065 | — | — | 1 | 6.55 |
| CHEMBL1951068 | — | — | 1 | 6.55 |
| CHEMBL430893 | (-)-ROLIPRAM | — | 1 | 6.30 |
| CHEMBL82318 | — | — | 1 | 6.28 |
| CHEMBL124706 | PHTHALAZINONE | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1951070 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL1951069 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL1951067 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL1951066 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL1951065 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1951068 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL430893 | (-)-ROLIPRAM | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL82318 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL124706 | PHTHALAZINONE | IC50 | = | 520.0 | nM | 6.28 |